TW541182B - Skin conditioning compositions containing an acid and a retinoid - Google Patents
Skin conditioning compositions containing an acid and a retinoid Download PDFInfo
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- TW541182B TW541182B TW086118988A TW86118988A TW541182B TW 541182 B TW541182 B TW 541182B TW 086118988 A TW086118988 A TW 086118988A TW 86118988 A TW86118988 A TW 86118988A TW 541182 B TW541182 B TW 541182B
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/67—Vitamins
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/67—Vitamins
- A61K8/671—Vitamin A; Derivatives thereof, e.g. ester of vitamin A acid, ester of retinol, retinol, retinal
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/30—Cosmetics or similar toiletry preparations characterised by the composition containing organic compounds
- A61K8/63—Steroids; Derivatives thereof
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K8/00—Cosmetics or similar toiletry preparations
- A61K8/18—Cosmetics or similar toiletry preparations characterised by the composition
- A61K8/72—Cosmetics or similar toiletry preparations characterised by the composition containing organic macromolecular compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/10—Anti-acne agents
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q17/00—Barrier preparations; Preparations brought into direct contact with the skin for affording protection against external influences, e.g. sunlight, X-rays or other harmful rays, corrosive materials, bacteria or insect stings
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/007—Preparations for dry skin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/02—Preparations for care of the skin for chemically bleaching or whitening the skin
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61Q—SPECIFIC USE OF COSMETICS OR SIMILAR TOILETRY PREPARATIONS
- A61Q19/00—Preparations for care of the skin
- A61Q19/08—Anti-ageing preparations
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Abstract
Description
541182 A7 經濟部中央標準局員工消費合作社印製 五、發明説明(2 生加成性抑制力,齊墩果酸及/或熊果酸與視網醇或視網 酉旨併用之效果,係類似於視網酸之效果,因此,齊墩果酸 及/或熊果酸與視網醇或視網酯之混合物於使用上較視網 酸容易且較為安全^ 本發明部分而言包含一種皮膚調理組合物,其包括: ⑻自約0.001%至約10%之類視色素,其選自由視網醇、 視網酯及彼等之混合物所組成之群; ⑸自約0.0001%至約50%、選自由齊墩果酸、熊果酸及 彼等之混合物所組成之群之化合物;以及 (c) 一種化妝品可接受媒液。 本發明進一步提供一種調理皮膚之化妝方法,包含局部 施:本發明之組合物於皮膚上。本發明亦提供一種模擬視 、’罔ix於皮膚上足功效的化妝方法,包含局部施用本發明之 組合物於皮膚上。 主本發明中之用語,,調理”,意指避免及處理一或多種下列 情形:乾燥型皮膚,光易傷害型皮膚,具皺紋之外表,老 人斑,老化肌膚。本發明之組合物亦有用於增加角質層之 美白皮膚,控制皮脂分泌,以及一般性地增加皮膚 該組合物亦可用以改善皮膚鱗片化以及表皮分生情 撓性質感 形。 輕佳具施例乏柄a 、:發明組合物中包含一種選自由視網醇、視網酯及彼 <此0物所組成(群的化合物,以作為第—必要成令。 -5- X 297公釐) (請先閱讀背面之注意事項再填寫本頁) 琴 訂 .會 541182 五、發明説明(3 ) f請先閲讀背面之注意事項再填寫本頁} 該用語"視網醇"除其餘已知種類之外尚包0 異構物.全-反-視網醇,13_順_視網醇,u_順·視 9-順-視網醇,3,4-二去氫-視網醇;較佳之 。, 反-視網醇,1 3-順·視網醇,%順·視網醇 - 網醇;最佳者係全-反-視網醇,因其係商業上可廣泛·^ 者。 又于 視網酯係視網醇之酯類,該用語”视網醇,,係如上所定 義。適用於本發明中之視網酯係視網醇之酯類,較 佳係其cvcw酯類,最佳係其&、&、及Cu酯類,因彼等 係商業上可最廣泛獲得者。視網酯之實例包括、但不限 於:棕櫚酸視網酯,甲醯視網酯,乙醯視網酯,丙醯視網 酯,丁醯視網酯,戊醯視網酯,異戊醯視網酯,己酮酸視 網酯,庚酮酸视網酯,辛酮酸視網酯,壬酮酸視網酯,癸 酮酸視網酯,十一酮酸視網酯,月桂酸視網酯,三癸酮酸 視網酯,十二酮酸視網酯,十五酮酸視網酯,十七酮酸視 網酯,硬脂酸視網酯,異硬脂酸視網酯,十九酮酸視網 酯’花生酸視網酯,山茶酸視網酯,羊毛酸視網酯,油酸 視網醋,視網醇内酯,乙二醇視網酯,羥己醯基視網酯, 肉桂醯基視網酉旨,酒石酸視網酉旨。 經淡,^中央標李局員工消費合作社印^ 本發明中所適用之較佳醇類,係選自棕櫚酸视網酶,甲 醯視網酯以及乙醯視網酯,因其係商業上最可廣泛獲得且 最便宜者。羊毛酸視網酯亦可使用,因其具備良好之功 效。 視網S旨及/或視網醋於本發明組合物中之用量,係自約 -6 - 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公缝) 541182 A7 B7五、發明説明(4 ) 0.001%至約10%,較佳係自約0.01%至約1%,最佳係自約 0.0 1 % 至約 0.5 %。 本發明組合物中所含之第二必要成分,係齊墩果酸、熊 果酸及彼等之混合物,此等酸具有下列結構: 經濟部中央標準局員工消費合作社印製541182 A7 Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs 5. Description of the invention (2 additive addition inhibition, oleanolic acid and / or ursolic acid combined with retinol or reticulum, similar effects In terms of the effect of retinoid, therefore, the mixture of oleanolic acid and / or ursolic acid and retinol or retinyl ester is easier and safer than retinoid ^ part of the present invention includes a skin conditioning A composition comprising: ⑻ from about 0.001% to about 10% of a retinoid, selected from the group consisting of retinol, retinyl esters, and mixtures thereof; ⑸ from about 0.0001% to about 50%, A compound selected from the group consisting of oleanolic acid, ursolic acid, and a mixture thereof; and (c) a cosmetically acceptable vehicle. The present invention further provides a cosmetic method for conditioning the skin, including topical application: The present invention The composition is on the skin. The present invention also provides a cosmetic method for simulating the effects of vision and feet on the skin, comprising topically applying the composition of the present invention to the skin. The term in the present invention, conditioning ", Means to avoid and deal with One or more of the following conditions: dry skin, light-prone skin, wrinkled appearance, age spots, aging skin. The composition of the present invention is also useful for increasing the whitening skin of the stratum corneum, controlling sebum secretion, and generally Increasing the skin The composition can also be used to improve the skin scaly and epidermal mesenchymal sensation. Lightness and goodness Examples Examples of lack of stem a: The composition of the invention contains one selected from the group consisting of retinol, retinyl ester, and ; This composition of 0 (group of compounds as the first necessary order. -5- X 297 mm) (Please read the precautions on the back before filling this page) Qin Ding. Meeting 541182 V. Description of the invention ( 3) f Please read the notes on the back before filling out this page} The term " visional alcohol " contains 0 isomers in addition to the rest of the known species. All-trans-resinol, 13_ 顺 _ Retinol, u_cis · retin-9-cis-retinol, 3,4-didehydro-retinol; better., Trans-retinol, 1 3-cis · retinol,% cis · Retinol-Retinol; the best is all-trans-retinol because it is commercially widely available. The esters of retinol, the term "retinol," is as defined above. The retinyl esters suitable for use in the present invention are the esters of retinol, preferably the cvcw esters, most preferably &;, &Amp;, and Cu esters, because they are the most widely available commercially. Examples of retinyl esters include, but are not limited to: retinyl palmitate, formamyl retinyl ester, and acetamyl retinyl ester , Propionate retinate, butyrate retinate, pentamate retinate, isoprene retinate, hexanoate retinoate, heptenoate retinate, octanoate retinate, nonanoic acid Retinyl esters, retinyl decanone, retinyl undecanoate, retinyl laurate, retinyl tridecanoate, retinyl dodecanoate, retinyl pentaketoate, ten Retinyl heptaestate, retinyl stearate, retinyl isostearate, retinyl nonadecanate, arachidic acid retinyl ester, camellic acid retinyl ester, lantic acid retinyl ester, oleic acid Retinol vinegar, retinol, ethylene glycol retinyl ester, hydroxycaproyl retinyl ester, cinnamyl retinyl ester, tartaric acid retinyl ester. According to the report, ^ printed by the Central Consumers Bureau Consumer Cooperative ^ The preferred alcohols applicable in the present invention are selected from the group consisting of palmitate retinase, formamyl retinyl ester, and acetamidine retinyl ester because they are commercially available. Most widely available and least expensive. Retinyl lanate can also be used because it has good effects. Vision S and / or the amount of Vision Vinegar in the composition of the present invention is from about -6-This paper size is applicable to Chinese National Standard (CNS) A4 specifications (210X297 cm) 541182 A7 B7 V. Description of the invention ( 4) 0.001% to about 10%, preferably from about 0.01% to about 1%, and most preferably from about 0.01% to about 0.5%. The second essential ingredient contained in the composition of the present invention is oleanolic acid, ursolic acid and their mixtures. These acids have the following structure: printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs
熊果酸 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) (請先閱讀背面之注意事項再填寫本頁) -裝· 訂 541182 五、發明説明(5 ) 應了解,依據組合物p Η > 、/ν 士從2人"丄 不同’齊墩果酸及/或熊果酸 於本發明組合物中可以鹽 …禾 趟存在。 式例如鹼金屬鹽或鹼土金屬 齊墩果酸及/或熊果酸於太 、本敖月組合物中之含量,係自約 0.0001%至約50%,較佳伤白从 你目、〇 从 係自約0.〇 1 %至約1 0%,最佳係自 約0 · 1 %至約5 %。 化·妝品可接香姓淦 本發明之組合物亦白本 . i η 一化妝品可接受媒液,以作為組 合物中活性成分之稀釋涂丨|、八 作拜釗、分散劑或載劑,是以,當其施 用於皮膚上時,可便利組合物之塗佈。 不同於水或者除了水以外之媒液,可包括液體或固體乳 化劑’溶劑,保濕劑,增稠劑及粉末。尤佳之非水性載劑 係聚二甲矽氧烷及/或聚二甲苯基矽氧烷ϋ明中適用 之矽酮係彼等於25°C下具有自10至10,000 mm2/s(分托)黏 度者,特別需要者係低黏度及高黏度矽酮之混合物,此等 矽酮係購自通用電子公司、商品名為VicasU把及SF者, 以及講自道康寧公司之200及50〇系列。矽酮於本發明組合 物中之用量,係佔組合物重之自約5 %至約9 5 %,較佳係自 約25%至約90%。 經濟部中央標準局員工消費合作社印製 (請先閱讀背面之注意事項再填寫本頁) 化妝品可接受媒液通常係佔組合物重之自約5%至約 99·9%,較佳係自約25%至約80%,且於無其他調整劑存 在下’可供補足組合物量之用。較佳地,媒液係為佔組合 物之至少5 0重量%、最佳係至少80重量%之水,較佳地, 本發明組合物中係含至少約5 〇重量%、最佳係自6 〇至8 〇重 -8 - 本紙張尺度適用中國國家標準(CNS ) Α4規格(210Χ297公釐) 541182 Α7 Β7 五、發明説明(6 ) 量%之水。 視需要添加之皮膚增益材料及化妝品調整劑 可存在油或者油性物質,以與乳化劑共同構成油包水乳 液或水包油乳液,此大部分取決於所使用乳化劑之平均親 水性-親脂性平衡值(HLB)。 本發明組合物中較佳包含防曬劑,防曬劑包括彼等一般 用以阻斷紫外線者。例示性之化合物如pABA、肉桂酸酯 及水楊酸酯之衍生物,例如,可使用辛基甲氧基肉桂酸酯 及2-羥-4-甲氧基苯基酚酮(即已知之氧基苯酮),辛基甲氧 基肉桂酸酯及2-羥-4-甲氧基苯基酚酮係商業上可獲得者, 商品名分別為Parsol MCX及Benzophen〇ne-3。乳液中所使 用的防曬劑之確實用量可依所欲的於太陽suv輻射下之保 護程度而改變。 另一種較佳之視需要成分係選自必須脂肪酸(EFAs), 即,彼等對所有細胞之血漿膜形成係屬必須之脂肪酸。當 角蛋白細胞EFA不足,會使細胞呈高預活化狀態,供應 EFA則可解決此節,EFA亦可提昇上皮細胞之磷脂生化合 成,並提供脂類於上皮細胞之障蔽形成。此必須脂肪酸較 佳係選自羊毛酸,γ-羊毛酸,同相羊毛酸,鈮酸,二十 石反-(η - 6,9,1 3)-二晞版’花生油埽酸,α _羊毛酸,二十碳五 晞酸,己烯酸及彼等之混合物。 尚有另一種較佳之視需要成分,其係選自吡咯類,例 如,順吡咯,雙颯吡咯,布三聚合吡咯,酮康絲吡咯,麥 康絲Ρ比嘻’依康絲Ρ比ρ各,印他康絲ρ比ρ各,說康絲ρ比嘻,二 -9 - 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) — J— I- -I m j I m · (請先閱讀背面之注意事項再填寫本頁) 訂 經濟部中央標準局員工消費合作社印製 541182 A7 B7 經濟部中央標準局員工消費合作社印製 五、發明説明( 聚康絲p比咯,丁氧康絲吡咯,硫康絲吡咯,尼龍康絲峨 咯,及彼等之混合物。吡咯於本發明組合物中之含量,可 為自約0.001%至約50%,較佳係自约〇 〇〇1%至約10%,最 佳係自約0.1%至約5%。 乳化劑係通常併入本發明化妝品組合物中者,此等乳化 劑可為總組合物自〇·5重量%至50重量%、較佳係介於$重 量%至30重量%之間。於一般化學分類中,乳化劑係歸類 為酯類,脂肪酸及醇,多元醇及烴。 酯類可為單-或二-酯類,可接受之脂肪酸二-酯類包括己 二酸二丁酯,癸二酸二乙酯,二異丙基二聚物,及琥珀酸 二辛酯;可接受之具支鏈脂肪酸酯包括2_乙基-己基十二烷 酉曰,硬爿曰鉍異丙酯,及棕櫚酸異硬脂酸酯;可接受之三鹼 酸醋包括三異丙基三羊毛酸酉旨及三月桂基擰權酸酉旨;可接 受之直鏈脂肪酸酯包括月桂基棕櫚酸醋,己内醯基十二 酯’油醯基幼克酯及硬脂酸油酸酯。較佳之酯類包括椰子 基辛酿醋/辛基酿(椰子基辛醯醋及椰子基辛基醋之混合 物)’丙=醇醚乙醯酯,=異丙基己醯酯及十六烷基辛酮 酉旨。 適當之脂肪酸及醇包括彼等具有1G至細碳原子之化合 物’此等化合物中特^去去#丄、 1者係十7T :!:元基、十二烷基、棕櫚基 及硬脂酸基醇及酸。 可作為乳化劑之多元醇係、線性及具支鍵垸基多經基化合 ::如,丙二醇’甘露醇及甘油係較佳者,亦可使用聚 &性夕元醇’例如聚丙二醇及聚乙二醇。丁二醇及丙二醇 本紙張尺度適财關家標 (請先閲讀背面之注意事項再填寫本頁) ·裝 II-----------r -10 - 541182 A7 B7 五、發明説明(8 係特佳可作為滲透加速劑者。 可作為乳化劑之烴類之例子,係彼等烴鏈上具有丨2至3 c 個碳原子者,特定之例子包括礦物油,石油膠,蜂膠及異 化白蠟油。 、 本發明之化妝品組合物中所含的其他類功能性成分係為 增稠劑,增稠劑通常存在佔組合物重之自〇1重量%至2〇重 =%,較佳係自0.5重量%至10重量%。增稠劑之例子為經 交聯之聚丙烯酸酯物質,可獲自B_F. G〇〇ddch公司,商品 名為Carbopol。可使用之膠係例如黃原膠,加連膠,凝 膠,刺梧桐膠,蛋白及大豆膠等。在特定之情況下,增稠 功能可藉由矽酮或乳化劑之添加來達成,例如,黏度超過 1〇分托之矽酮膠,以及具有雙重功能的如硬脂酸甘油酯等 酯類。 粉末亦可併入本發明之化妝品組合物中,此等粉末包 括丄白咢粉,滑石粉,高嶺土,澱粉,齊黏土,經過化學 改質之鎂鋁矽酸鹽,經過有機性改質之蒙托土,水合矽酸 鋁,發煙矽石,鋁澱粉辛醯基琥珀酸酯,以及彼等之混合 物。 經濟部中央標準局員工消費合作社印製 (請先閲讀背面之注意事項再填寫本頁) 訂 其他調整劑次要成分亦可併入本發明之化妝品组合物 中,此等成分包括著色劑,珠光劑及香水,此等其餘&整 劑次要成分之用量可佔組合物重之自〇 〇〇1重量%至言 〇 重量%。 局、 粗合物之使用 本發明之化妝品組合物主要係欲作為局部施用於人 -11 - 541182 Α7Ursolic acid paper size applies Chinese National Standard (CNS) A4 specification (210X297 mm) (Please read the precautions on the back before filling this page)-Binding and binding 541182 V. Description of the invention (5) It should be understood according to the combination The properties p Η > and / ν are from 2 people " 丄 different 'oleanolic acid and / or ursolic acid in the composition of the present invention may be salt ... glutamate. For example, the content of the alkali metal salt or alkaline earth metal oleanolic acid and / or ursolic acid in the composition of Tai and Ben Ao Yue is from about 0.0001% to about 50%. The range is from about 0.01% to about 10%, and the best range is from about 0.1% to about 5%. Cosmetics and cosmetics can be added to the composition of the present invention. The composition of the present invention is also innocuous. I η is a cosmetic acceptable vehicle, which is used as a diluent for the active ingredients in the composition. Therefore, when it is applied to the skin, the application of the composition can be facilitated. Other than water or vehicles other than water, liquid or solid emulsifiers' solvents, humectants, thickeners and powders can be included. Particularly preferred non-aqueous carriers are silicones suitable for use in polydimethylsiloxane and / or polyxylylsiloxane, which have a temperature of from 10 to 10,000 mm2 / s at 25 ° C. Those with viscosity, especially those who need it are mixtures of low-viscosity and high-viscosity silicones. These silicones were purchased from General Electronics, trade names VicasU and SF, and 200 and 50 series from Dow Corning. The amount of silicone used in the composition of the present invention is from about 5% to about 95% by weight of the composition, preferably from about 25% to about 90%. Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling this page). The acceptable media for cosmetics usually account for about 5% to about 99.9% of the weight of the composition, preferably from From about 25% to about 80%, and 'to make up the amount of the composition in the absence of other modifiers. Preferably, the vehicle solution is at least 50% by weight of the composition, and most preferably at least 80% by weight of the composition. Preferably, the composition of the present invention contains at least about 50% by weight, most preferably 60 to 800 weight-8-This paper size applies to Chinese National Standard (CNS) A4 specification (210 × 297 mm) 541182 Α7 B7 5. Description of the invention (6) Amount of water. Skin gain materials and cosmetic conditioners added as needed may contain oil or oily substances to form a water-in-oil emulsion or oil-in-water emulsion together with the emulsifier, which mostly depends on the average hydrophilicity-lipophilicity of the emulsifier used Balance value (HLB). The compositions of the present invention preferably include sunscreen agents, including those commonly used to block ultraviolet rays. Exemplary compounds such as derivatives of pABA, cinnamate and salicylate, for example, octylmethoxycinnamate and 2-hydroxy-4-methoxyphenylphenol ketone (known as oxygen Acetophenone), octylmethoxycinnamate and 2-hydroxy-4-methoxyphenylphenol ketone are commercially available under the trade names Parsol MCX and Benzophenone-3, respectively. The exact amount of sunscreen used in the emulsion may vary depending on the desired degree of protection from solar suv radiation. Another preferred optional ingredient is selected from essential fatty acids (EFAs), that is, they are essential fatty acids for plasma membrane formation of all cells. When the EFA of keratinocytes is insufficient, the cells will be in a high pre-activated state. Supplying EFA can solve this problem. EFA can also enhance the phospholipid biosynthesis of epithelial cells and provide the barrier formation of lipids in epithelial cells. This essential fatty acid is preferably selected from the group consisting of lantic acid, γ-lanic acid, homophagic lantic acid, niobic acid, icos- stone trans- (η-6,9,1 3) -dihydrazone version of arachidonic acid, α_wool Acid, eicosapentapentanoic acid, hexenoic acid and mixtures thereof. There is still another preferred ingredient as needed, which is selected from the group of azoles, for example, cis-pyrrole, bispyrrole, cloth trimer pyrrole, ketoconazole, mcconsylpyrrolidone, and ekonsylpyrazole. , Intacons ρ ratio ρ, said Kang Si ρ ratio, 2-9-This paper size applies Chinese National Standard (CNS) A4 specifications (210X 297 mm) — J— I- -I mj I m · (Please read the notes on the back before filling out this page) Order printed by the Central Consumers ’Cooperative of the Ministry of Economic Affairs printed by 541182 A7 B7 Printed by the Central Consumers’ Cooperative of the Ministry of Economic Affairs printed by the Consumer Cooperative of the Ministry of Economic Affairs Oxyconsyl pyrrol, thioconsyl pyrrol, nylon consiole, and mixtures thereof. The content of pyrrole in the composition of the present invention may be from about 0.001% to about 50%, preferably from about 0.00%. 〇1% to about 10%, preferably from about 0.1% to about 5%. Emulsifiers are generally incorporated into the cosmetic composition of the present invention, and these emulsifiers can be from 0.5% to 5% by weight of the total composition 50% by weight, preferably between $% and 30% by weight. In general chemical classification, emulsifiers Classified as esters, fatty acids and alcohols, polyhydric alcohols and hydrocarbons. Esters can be mono- or di-esters, and acceptable di-esters of fatty acids include dibutyl adipate, diethyl sebacate, Diisopropyl dimer, and dioctyl succinate; acceptable branched fatty acid esters include 2-ethyl-hexyldodecane, bismuth isopropyl ester, and isostearic palmitate Fatty acid esters; acceptable tribasic acid esters include triisopropyltrilanic acid and trilauryl glutamic acid; acceptable linear fatty acid esters include lauryl palmitate and caproyl Dodecyl esters of oleyl oleate and stearic acid oleate. Preferred esters include coconut-based vinegar / octyl vinegar (a mixture of coconut-based octyl vinegar and coconut-based octyl vinegar) 'c = Alcohol ether ethyl ester, = isopropylhexanoate and hexadecyl octanone. Suitable fatty acids and alcohols include those compounds having 1G to fine carbon atoms. Among these compounds ^ 去去 # 丄1, 1 is ten 7T:!: Yuan group, dodecyl group, palmity group and stearic alcohol and acid. Polyol series, linear and branched, which can be used as emulsifier. Polyalkylene-based compound: For example, propylene glycol 'mannitol and glycerol are better, and poly & alcohols such as polypropylene glycol and polyethylene glycol. Butylene glycol and propylene glycol are suitable for this paper Guan Jiabiao (Please read the precautions on the back before filling out this page) · Install II ----------- r -10-541182 A7 B7 V. Description of the invention (8-series special good can be used as penetration accelerator Examples of hydrocarbons that can be used as emulsifiers are those having 2 to 3 c carbon atoms in their hydrocarbon chains. Specific examples include mineral oil, petroleum gum, propolis, and dissimilated ash oil. The cosmetic composition of the present invention The other functional ingredients contained in the composition are thickeners. Thickeners usually exist in the range of from 0.01% to 20% by weight of the composition, preferably from 0.5% to 10% by weight. An example of a thickener is a cross-linked polyacrylate material, available from B.F. Godddd, under the trade name Carbopol. Examples of gums that can be used include xanthan gum, gellan gum, gelatin, sycamore gum, protein and soybean gum. Under certain circumstances, thickening can be achieved by the addition of silicone or emulsifiers, such as silicone gums with a viscosity of more than 10 d Torr, and esters with dual functions such as glyceryl stearate. Powders can also be incorporated into the cosmetic composition of the present invention. These powders include scallion powder, talc, kaolin, starch, homogeneous clay, chemically modified magnesium aluminosilicate, and organically modified magnesium Supporting clay, hydrated aluminum silicate, fumed silica, aluminum starch octyl succinate, and mixtures thereof. Printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (please read the precautions on the back before filling this page) Order other modifiers. The minor ingredients can also be incorporated into the cosmetic composition of the present invention. These ingredients include colorants, pearlescent Agents and perfumes, and the amount of these remaining & whole ingredients minor components may range from 0.001% to 0% by weight of the composition. Use of local and crude compounds The cosmetic composition of the present invention is mainly intended for topical application to humans -11-541182 Α7
經濟部中央標準局員工消費合作社印製 :上之製品,尤其欲作為條理皮膚及 降低敏紋或老化皮膚之.外表之製劑。 州 -使广二’係將小量之组合物(例如1至1〇〇毫升)自適當之 Μ或使用器取出並施用於皮膚外露之區域,1,若兩 要’以手或手指或適當之裝置均勾塗佈及/或塗抹於皮二 上。 月 製品形式及电常 本1月之局部皮膚處理組合物可適當地調配成乳液、+ 或,三此組合物可依消費者之需求及配合其黏度包裝於適 當容器中,例^,乳液或霜可包裝於瓶子或滾球使用器 Ί喷霧推進喷霧裝置巾,或者接有適於手指操作的絮 浦足容器中,當組合物為霜時,僅可以儲存於不變形之瓶 子或擠出瓶中,例如試管或加蓋噴霧器。 此組合物亦可包裝於彼等例如描述於美國專利第 5,063,057號之膠囊中。 因此,本發明亦提供一種如本文中所定義的含有化妝上 可接受組合物之密閉容器。 下列特定實例進一步例示本發明。 材料及方法 細胞培巷 將人類角蛋白細胞(經胰蛋白酶處理並單離自新生兒前額 肌膚)於〇1!丨3€(:〇〇改質液(〇]\1£)^^1115?12(1:1)介質/1〇% 胎牛血漿中、及於經照射之小鼠成纖維細胞之存在下進行 培養,以建立各別的角蛋白細胞複製體,將細胞於上述條 12- 本紙張尺度適用中國國家標準(CNS) Α4規格(210Χ 297公釐) (請先閲讀背面之注意事項再填寫本頁} 裝 訂 541182 經濟部中央標準局員工消費合作社印製 Α7 Β7 五、發明説明(ι〇) 件下培養,直至第二傳代產生為止,然後將之冷凍備用。 在替換至購自Clonetics公司(San Diego,CA)的含〇」5 mM #5之無血漿MCDB 153基底介質角蛋白細胞增生介質 (KGM)、或者購自GIBCO公司的含0.09 mM#5之無角蛋白 細胞介質(KSFM)之前,先將冷凍之第二傳代角蛋白細胞溶 化並植入上述介質中,並繼續培養5天。第7天時,當細胞 已有80-9 0%匯合後,將之予以胰蛋白化並植入無血漿介質 中進行許多不同試驗。 轉谷胺醯胳gfeaij定 轉谷胺醯胺醃測定輿角蚤白細胞之合化 在上皮細胞之最終分化過程,1 5 nm厚之蛋白質層(已知 之角化套(CE))係形成於細胞外型之内面,ce係由許多不 同之蛋白質所構成,由於經至少一種上皮細胞中之轉谷胺 酿胺酶(TGases)之催化作用形成Nε-(γ-谷胺醯胺基)賴胺酸 異二胜肽鍵而交聯鍵結在一起。轉谷胺醯胺酶丨〇 係豐藏於上皮細胞之分化層中,尤其係柱狀層,然不存在 於未分化之基礎上皮細胞層中,因此,轉谷胺醯胺酶I係 上皮角蛋白細胞分化作用取有用之產生源,高TGasesj含 量代表更多的分化狀態。以ELISA為主之TGases測定(使用 TGases I抗體)係用以分析下列實例中經培養之角蛋白細胞 之分化狀態。 就實例1而言,係利用以下操作程序: 將角蛋白細胞(經上述方法培養)植入96個井狀盤中,其 密度須為每200 μΐ介質每井中有3,〇〇〇個細胞。待培養4天 -13 - 本紙張尺度適用中國國家標準(CNS ) Α4規格(210X 297公餐) (請先閲讀背面之注意事項再填寫本頁} 訂 541182 A7 B7 五、發明説明(11 經濟部中央標準局員工消費合作社印製 後更換介質為含有測試物質(每次測試用6個複製品)之介 質,於另外的72小時後,介質係經發氣,並將平盤儲存 於-70°C下。自冷凍器中移出平盤,並以pBS清洗細胞,添 加100 μΐ之消毒水,將細胞於_7〇°c下冷凍以進行冷凍再造 然後溶化。細胞係於室溫(R/T)下以pbs/3% BSA(清洗緩 衝液,牛血液樣本)培養丨小時,然後以新的清洗緩衝液洗 滌。以購自Biomedical公司、經以i : 2,000清洗緩衝液稀 釋之第抗骨·^單複製體抗人體谷胺醯胺酶小藏抗體(igG) 於-3 7 °C下培養1小時,然後以清洗緩衝液清洗2次。接著 以50 μΐ的經以i : 4,000清洗緩衝液稀釋之第二抗體(17礼殘 段,過氧化酶共軛抗小白鼠IgG,購自Amersham公司)於 37°C下培養1小時,然後以清洗緩衝液清洗2次。以基底溶 液(4耄克鄰-苯晞二胺及3 3…的3〇% ^⑺於1〇毫升〇」μ 檸檬酸酯中緩衝至pH 5.0)於室溫(R/T)下及黑暗中(以鋁泊 包住)培養細胞5分鐘,添加50 (^的4N h2S〇4後反應停 止。於492 nm處自平盤讀出計上讀出樣本之吸收度,在6 個複製樣本中,將4個以兩種抗體處理,另2個僅以第二抗 骨豆處理(即,測定鍵結酵素共軛Ab之背景)。TGases係利用 每次處理扣除背景校正所得之讀數定之,並記錄曝置於兩 種抗體中的平均值土s.d.。 於實例2中,係利用以下操作程序: 將角蛋白細胞(經上述方法培養)植入9 6個井狀盤中,其 密度須為每200 μΐ介質每井中有3,〇〇〇個細胞。待培養4天 後更換介貝為含有測試物質(每次測試用6個複製品)之介 -14 本纸張尺度適用中國國家標·準(CNS ) Α4規格(210Χ 297公慶) (請先閱讀背面之注意事項再填寫本頁) β Γ Ρ 541182 A7 ____B7 五、發明説明(12 ) 質’於另外的7 2小時後,介質係經發氣,並將平盤儲存 於-70 °C下。自冷凍器中移出平盤,並以pBS清洗細胞3 次’添加100 μΐ之消毒水,將細胞於_7〇°CT冷凍以進行冷 凍再造然後溶化。細胞係於室溫(R/T)下以pBS/3% BSA( /目洗緩衝液’牛血液樣本)培養1小時,然後以新的 清洗緩衝液洗滌。以購自B i 〇 m e d i c a 1公司、經以1 : 2,〇 〇 〇 清洗緩衝液稀釋之第一抗體單複製體抗人體谷胺醯胺酶小 鼠抗體(IgG)於-37°C下培養1小時,然後以清洗緩衝液清洗 2次。接著以50 μΐ的經以1 : 4,000清洗緩衝液稀釋之第二 抗體(Fab殘段,過氧化酶共軛抗小白鼠IgG,講自 Amersham公司)於37°C下培養1小時,然後以清洗緩衝液 清洗2次。以基底溶液(4毫克鄰-苯晞二胺及3·3 μ1的3〇0/〇 Η2〇2於10毫升(Μ μ擰檬酸酯中緩衝至pH 5.0)於室溫(r/丁) 下及黑暗中(以铭泊包住)培養細胞5分鐘,添加5 0 μ 1的4N ΗΘ〇4後反應停止。於492 nm處自平盤讀出計上讀出樣本 之吸收度,在6個複製樣本中,將4個以兩種抗體處理,另 2個僅以第二抗體處理(即,測定键結酵素共軛Ab之背 景)。轉谷胺醯胺酶之測定係利用每次處理扣除背景校正 經濟部中央標準局員工消費合作社印製 (請先閲讀背面之注意事項再填寫本頁) 所得之讀數定之,並記錄曝置於兩種抗體中的平均值 土 s · d · ° DNA測定 經細胞處理後之TGase I測定會受到細胞數目之影響,亦 即,細胞數目越多,測得之TGase-1量便越多。利用將相 同井中TGase I之量正常化至與細胞之DNA含量相同,便 -15- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 541182 A7 B7 五、發明説明(13) (請先閱讀背面之注意事項再填寫本頁) 可消除因為細胞數目不同造成之變異。DNA量係細胞數目 特別有用之指標,包括對角蛋白細胞而言亦然,因為各個 細胞皆有其本身之功能及相同之基因組,因此可定出DNA 之量。細胞壁之DNA總量,係直接正比於細胞壁中之細胞 數目’ DNA之定量係用以正常化TGase之數值至細胞數 目。 將角蛋白細胞植入96個井狀盤中,其密度需為每200 μΐ 介溢母井中含有3,000個細胞。待培養4天後更換介質為含 有測減物質(每次測試用6個複製品)之介質,於另外的7 2 小時後,介質係經發氣,並將平盤儲存於-70。(:下至少1.5 小時。將平盤自冷凍器中移出並溶化3〇分鐘。添加1 〇〇 μΐ 的Hoechst染料(1 μΐ/ml最終濃度),然後培養細胞15分鐘, 蓋上並自螢光計中讀出吸收度(360 nm及460 nm)。移出染 料溶液,並以測定TGase中所製備之PBS清洗培養井。 1Γ例1 於改變角蛋白細胞之分生作用狀態,視網酸比視網薄#有 添加視網酸(RA)及視網醇(R0H)後、對轉谷胺醯胺酶量 正常化至細胞DNA含量之影響係經測試,列於表1中。 經濟部中央標準局員工消費合作社印製 準 標 !家 國 I國 I中 用 -£ J度 一尺 張 紙 I本Printed by the Consumer Cooperatives of the Central Standards Bureau of the Ministry of Economic Affairs: The above products are especially intended to be used as skin care and reduce the appearance of sensitive skin or aging skin. State-Yangguang 'is to take a small amount of the composition (for example, 1 to 100 ml) from a suitable M or a device and apply it to the exposed area of the skin. The devices are all hook-coated and / or smeared on the second skin. In the form of monthly products, the topical skin treatment composition in January can be appropriately formulated into an emulsion, + or three. The composition can be packaged in an appropriate container according to the needs of the consumer and its viscosity, for example, emulsion or The cream can be packaged in a bottle or a roller ball using a spray-propulsion spray device towel, or in a container suitable for finger operation. When the composition is a cream, it can only be stored in a non-deformed bottle or squeezed. Out of the bottle, such as a test tube or capped sprayer. This composition can also be packaged in capsules such as those described in U.S. Patent No. 5,063,057. Accordingly, the present invention also provides a closed container containing a cosmetically acceptable composition as defined herein. The following specific examples further illustrate the invention. Materials and methods Cell culture lanes human keratin cells (treated with trypsin and isolated from the forehead skin of newborns) at 〇1! 丨 3 € (: 〇〇 conditioner (〇) \ 1 £) ^^ 1115 ? 12 (1: 1) medium / 10% fetal bovine plasma and cultured in the presence of irradiated mouse fibroblasts to establish individual keratinocyte replicas. -This paper size is in accordance with Chinese National Standard (CNS) A4 specification (210 × 297 mm) (Please read the precautions on the back before filling out this page} Binding 541182 Printed by the Staff Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs (Ι〇) incubate until the second passage, and then frozen for later use. Replaced with 0 "5 mM # 5 plasma-free MCDB 153 base medium purchased from Clonetics (San Diego, CA). Keratinocyte Proliferation Medium (KGM), or 0.09 mM # 5 keratin-free cell medium (KSFM) purchased from GIBCO, first dissolve frozen second-passage keratin cells and implant into the above media, And continue to culture for 5 days. On the 7th day, when the cells have 8 After 0-9 0% confluence, they were trypsinized and implanted in plasma-free medium for many different tests. Transglutamine 醯 gfeaij was determined to be transglutamine marinated to determine the integration of C. lepidium leukocytes in epithelial cells In the final differentiation process, a 15-nm-thick protein layer (known as keratinocytes (CE)) is formed on the inner surface of the outer cell shape, and ce is composed of many different proteins. Glutamine enzymes (TGases) catalyze the formation of Nε- (γ-glutamine amino) lysine isodipeptide bonds and cross-linking bonds together. Transglutaminase 丨 0 is a rich store In the differentiated layer of epithelial cells, especially the columnar layer, it does not exist in the undifferentiated base epithelial layer. Therefore, transglutaminase I is a useful source for the differentiation of epithelial keratin cells. The TGasesj content represents more differentiation status. The ELISA-based TGases assay (using TGases I antibody) is used to analyze the differentiation status of the cultured keratin cells in the following examples. For Example 1, the following procedure was used : Put keratin cells ( Cultured in the above method) Implanted into 96 wells with a density of 3,000 cells per 200 μΐ medium per well. To be cultured for 4 days-13-This paper is in accordance with Chinese National Standard (CNS) Α4 Specifications (210X 297 meals) (Please read the precautions on the back before filling out this page} Order 541182 A7 B7 V. Invention Description (11 Printed by the Consumer Standards Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs, replace the medium with a test substance (each time Six replicates of the test medium were used. After another 72 hours, the medium was aerated and the flat disks were stored at -70 ° C. Remove the plate from the freezer, wash the cells with pBS, add 100 μΐ of sterilized water, freeze the cells at -70 ° C for freeze-reconstitution, and then dissolve. Cell lines were incubated at room temperature (R / T) with pbs / 3% BSA (washing buffer, bovine blood samples) for one hour, and then washed with fresh washing buffer. The first anti-bone · ^ single replica anti-human glutamine synthetase antibody (igG) purchased from Biomedical Company and diluted with i: 2,000 washing buffer was incubated at -37 ° C for 1 hour, and then Wash twice with washing buffer. Then, 50 μΐ of secondary antibody diluted in i: 4,000 washing buffer (17 sera, peroxidase-conjugated anti-mouse mouse IgG, purchased from Amersham) was cultured at 37 ° C for 1 hour, and then Wash twice with washing buffer. Base solution (4 g of ortho-phenylenediamine and 30% of 3 3… in 10 ml of 0 ″ μ citrate buffered to pH 5.0) at room temperature (R / T) and dark The cells were cultured for 5 minutes in medium (encapsulated with aluminum pod), and the reaction was stopped after the addition of 50 μ 的 of 4N h2SO4. The absorbance of the sample was read from a flat-panel readout meter at 492 nm. In 6 replicate samples, Four were treated with two antibodies, and the other two were treated only with the second anti-osteoporosis (ie, the background of the bound enzyme conjugate Ab was determined). TGases were determined by subtracting the background correction readings from each treatment and recorded The average value sd of exposure to the two antibodies. In Example 2, the following procedure was used: Keratin cells (cultured as described above) were implanted into 96 well-shaped dishes, the density of which must be 200 per 200 There are 3,000 cells in each well of the μΐ medium. After 4 days of culture, the medium is replaced with a medium containing a test substance (6 copies for each test). -14 CNS) Α4 specification (210 × 297 public holidays) (Please read the precautions on the back before filling this page) β Γ Ρ 541182 A7 _ ___B7 V. Description of the invention (12) After another 7 2 hours, the medium is aerated and the pan is stored at -70 ° C. Remove the pan from the freezer and wash the cells with pBS 3 Add 100 μΐ of sterilized water, freeze the cells at _70 ° CT for freezing and reconstitution, and then lyse. The cell line was incubated at room temperature (R / T) with pBS / 3% BSA (/ eye wash buffer). (Blood sample) for 1 hour, and then washed with a new washing buffer. The first antibody single replica anti-human glutamine was purchased from Biomedica 1 and diluted with a washing buffer of 1: 2,000. The amylase mouse antibody (IgG) was cultured at -37 ° C for 1 hour, and then washed twice with washing buffer. Then, 50 μΐ of a second antibody (Fab residue was diluted with 1: 4,000 washing buffer) , Peroxidase-conjugated anti-mouse IgG, from Amersham) was incubated at 37 ° C for 1 hour, and then washed twice with washing buffer. The base solution (4 mg of o-phenylenediamine and 3 · 3 μ1 of 300 / 〇2〇2 in 10 ml (M μ buffered citrate to pH 5.0) at room temperature (r / butyl) and in the dark The cells were cultured for 5 minutes, and the reaction was stopped after adding 50 μ 1 of 4N ΗΘ〇4. The absorbance of the sample was read from a flat-plate reader at 492 nm. 4 were treated with two antibodies, and the other 2 were treated with only the second antibody (ie, the background of the binding enzyme conjugate Ab was determined). The measurement of transglutaminase was performed by subtracting the background correction for each treatment from the center of the Ministry of Economic Affairs Printed by the Consumer Bureau of Standards Bureau (please read the precautions on the back before filling out this page) The readings obtained are determined, and the average value of the exposure to the two antibodies is recorded. S · d · ° DNA measurement after cell processing The TGase I assay is affected by the number of cells, that is, the larger the number of cells, the greater the amount of TGase-1 measured. By normalizing the amount of TGase I in the same well to the same DNA content as the cells, -15- This paper size applies the Chinese National Standard (CNS) A4 specification (210X297 mm) 541182 A7 B7 V. Description of the invention (13) ( (Please read the notes on the back before filling out this page) to eliminate the variation caused by the number of cells. The amount of DNA is a particularly useful indicator of the number of cells, including also for keratin cells, because each cell has its own function and the same genome, so the amount of DNA can be determined. The total amount of DNA in the cell wall is directly proportional to the number of cells in the cell wall. The quantification of DNA is used to normalize the value of TGase to the number of cells. Keratin cells are implanted into 96 well-shaped dishes at a density of 3,000 cells per 200 μΐ mediated overflow wells. After 4 days of incubation, the medium was replaced with a medium containing reduced substances (6 replicates for each test). After another 72 hours, the medium was aerated and the flat disk was stored at -70. (: At least 1.5 hours. Remove the plate from the freezer and dissolve for 30 minutes. Add 100 μΐ Hoechst dye (1 μΐ / ml final concentration), then culture the cells for 15 minutes, cover and autofluorescence Read the absorbance in the meter (360 nm and 460 nm). Remove the dye solution and wash the culture wells with the PBS prepared in TGase. 1Γ Example 1 To change the meristematic state of keratin cells, compare with retic acid网 薄 # With the addition of retinoid (RA) and retinol (ROH), the effects of normalizing the amount of transglutaminase to the cell's DNA content have been tested and are listed in Table 1. Central Standards of the Ministry of Economic Affairs Bureau Consumer Consumption Cooperative Prints Proper Standards! Home Country I Country I Use-£ J Degree One Foot Sheet of Paper I
S N 541182S N 541182
AA
7 B 五、發明説明(14) 經濟部中央標準局員工消費合作社印製7 B V. Description of the Invention (14) Printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs
CSJ CO NJ CsJ CsJ pr LH X f—' 〇 υτ X ι—* 〇 LH X H-1 〇 X >-1 〇 LH X H-* 〇 LH X 0 1¾ 二 2: 2Γ 3f 二 3: 2Γ 刀 〇 > 73 O > 70 q > CO Ο !+ ο υτ Ό Η C0 1+ ο \D CD Ι-τ ο UJ 0 LJ 二 H· 0 二 o l—1 £ 〇 fO Cvj 0 H* 0 !-* i—1 CO A A Ι ο CO A 0 -T4 丨+上怎 00 CL H /·s C') *JU- CJ hr.* ^ σ V ·— Ο c*P c*P LH c9 Cf> w b 0 〇N〇 X ο ο ο Η 〇 o o M 〇 〇 〇 〇 〇 〇 〇 〇 〇 l—1 〇 〇 〇 1 < CO -=]? ο ο ο Η o o o h-4 0 0 0 1—1 〇 fO 1 〇 〇 〇 H-1 0 0 0 !-* —Ό ^ < ^ Μ Ο ίο X ο o 0 0 〇 〇 一 Ό % <:. ο ο Η CD 二 1 0 0 H-* 0 0 〇 〇 〇 〇 1-* 73⑺ 〇 IJ 丄 Οι X o 0 〇 〇 〇 0 0 二二 1 o 〇 0 0 H-* 0 0 ι-* 〇 Η* 0 — Ο ΙΟ —ο. X -17- (請先閱讀背面之注意事項再填寫本頁) 訂 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 541182 A7 B7 五、發明説明(15) 所有經測試之視網酸濃度,即,2 5 χ 1〇-7 Μ,2·5 X 1〇-8 Μ,2 · 5 X 1 Ο Μ,相對於乙醇控制組而言,降低了角蛋白 細胞之分生作用,而就每一個相關濃度·· 2·5χ 1〇-7 Μ,2.5 X ΙΟ·8 Μ,2·5 X 10_9 Μ視網醇處理而言,其改良度亦增 加。轉谷胺醯胺酶含量之減少係取決於視網酸及視網醇之 劑量,此與於改變角蛋白細胞分生狀態下、視網酸比視網 醇更有效之論點一致。 會例2CSJ CO NJ CsJ CsJ pr LH X f— '〇υτ X ι— * 〇LH X H-1 〇X > -1 〇LH X H- * 〇LH X 0 1¾ 22: 2Γ 3f 22: 2Γ knife 〇 > 73 O > 70 q > CO Ο! + Ο υτ Ό Η C0 1+ ο \ D CD Ι-τ ο UJ 0 LJ two H · 0 two ol-1 £ 〇fO Cvj 0 H * 0! -* i—1 CO AA Ι ο CO A 0 -T4 丨 + 上 how 00 CL H / · s C ') * JU- CJ hr. * ^ σ V · — 〇 c * P c * P LH c9 Cf > wb 0 〇N〇X ο ο ο Η 〇oo M 〇〇〇〇〇〇〇〇〇〇1—1 〇〇〇1 < CO-=]? ο ο ο Η ooo h-4 0 0 0 1-1 〇fO 1 〇〇〇H-1 0 0 0!-* —Ό ^ < ^ Μ Ο ίο X ο o 0 0 〇〇 一 Ό% < :: ο ο Η CD 2 1 0 0 H- * 0 0 〇〇〇〇〇1- * 73⑺ 〇IJ 丄 Οι X o 0 〇〇〇〇0 222 1 o 〇0 0 H- * 0 0 ι- * 〇Η * 0 — 〇 ΙΟ —ο. X -17- (Please read the precautions on the back before filling this page) The size of the paper used for this edition applies to the Chinese National Standard (CNS) A4 (210X297 mm) 541182 A7 B7 V. Description of the invention 15) All tested retinoic acid concentrations, ie, 2 5 χ 1〇-7 Μ, 2.5 X 1 〇-8 Μ, 2.5 χ 10 Μ, compared to the ethanol control group, reduced The meristematic effect of keratin cells, and for each relevant concentration ····· 5χ 10-7 M, 2.5 X 10 · 8 M, 2 · 5 X 10-9 M, as far as retinol treatment, its degree of improvement also increased . The reduction in transglutaminase content depends on the doses of retinoid and retinol, which is consistent with the argument that retinoid is more effective than retinol in changing the keratinocyte meristem state. Session 2
齊壤一果酸與視網移可如成性抑射角蛋白細胞之分化作I 對TGase I量正常化至細胞DNA含量之影響係以相關於經 以測試化合物進行72小時處理後始測定之,結果係列於表 2中。 (請先閲讀背面之注意事項再填寫本頁) 訂 Φ 經濟部中央標準局員工消費合作社印製 本紙張尺度適用中國國家標準(CNS ) A4規格(210X297公釐) 541182 五、發明説明(17) 由表2中之數據可知,2·5χ 1 〇-7Μ<視網酸對壓抑角質化 TGase I含量相當有效(相對於44控制%而言),2 5χι〇_7Μ 之視網醇比視網酸無效,而丨〇·6μ之齊墩果酸當單獨使用 時^對角質化TGase I含量不具抑制力。然2·5χι〇-7Μ之視 網醇+ ίο 6μ <齊墩果酸抑制角質化TGase Γ含量至控 制量,因此,齊墩果酸與視網醇對角蛋白細胞分化作用具 有類似於視網酸功效之加成性效果。 八 於實例1至2中,視網酸係作為正控制組以及與其餘化合 物分析比較纟參考組。視網§交,於一定劑量下可降低皮膚 角蛋白細胞中之轉谷胺酿胺酶含量,換言之,視網酸可^ 低角蛋白細胞之分化作用。於抑制角蛋白細胞之分化作用 万面,視網醇及棕櫊酸視網酯很明顯地較視網酸無效。 經濟部中央標準局員工消費合作社印製 上述實例所表現之非可預期功效在於:視網醇或視網酉旨 對培養角蛋白細胞之影響力可大為提昇至接近視網酸者, 其係藉由將視網醇或酯與佔組合物重自約〇〇〇〇1%至約 5〇%之一種化合物併用而達成,其中該化合物經由活體外 微粒體測定顯示於100_之濃度下、可抑制至少2〇%的由 ^RAT或ARAT催化之视網酯化反應。此等功效並非僅大於 單獨使用視網醇或其酯類者,且大於併用此兩種成分以對 角蛋白細胞產生類似於視網酸功效的加成性功效者。 實例3-8係例示本發明之組合物,此等組合物可依習知方 法製備’其係適合於化妝品用途’尤其,此等組合物係適 合於级紋、粗縫、乾燥、裂開、老化幻或經…傷害之皮 膚之用途中,以改善皮膚外觀及觸感,本發明之組合物適 -20- 本纸張尺iUiTssi家標準(CNS )7^721GX297公釐) 541182The effect of homoacid and retinoic acid on the differentiation of adult keratinocytes as normal I on TGase I normalization to cellular DNA content is related to the determination after 72 hours of treatment with test compounds. The result series are shown in Table 2. (Please read the precautions on the back before filling out this page) Order Φ Printed by the Central Consumers Bureau of the Ministry of Economic Affairs, printed by the Consumer Cooperative, the paper size is applicable to the Chinese National Standard (CNS) A4 specification (210X297 mm) 541182 5. Description of the invention (17) From the data in Table 2, it can be seen that 2.5 × 1 0-7M < retinoic acid is quite effective in suppressing keratinizing TGase I content (relative to 44% of control), and 2 × χ〇_7M is more effective than sight The acid is ineffective, and oleanolic acid of 0.6 μ when used alone has no inhibitory effect on keratinized TGase I content. However, 2 · 5χι〇-7M of retinol + 6 μ < oleanolic acid inhibits keratinization TGase Γ content to a controlled amount. Therefore, oleanolic acid and retinol have similar effects on keratinocyte differentiation Additive effect of net acid effect. In Examples 1 to 2, retinoids were used as the positive control group and compared with the rest of the compound analysis 纟 reference group. Vision § cross, at a certain dose can reduce the content of transglutaminase in skin keratin cells, in other words, retinoic acid can reduce the differentiation of low keratin cells. In inhibiting the differentiation of keratin cells, retinol and retinyl palmitate are obviously less effective than retinoid. The unpredictable effect of the above example printed by the Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs is that the influence of retinol or retinol on cultured keratin cells can be greatly increased to those close to retinoid, which This is achieved by combining retinol or an ester with a compound that weighs from about 0.0001% to about 50% of the composition, wherein the compound is shown by in vitro microsomal assays at a concentration of 100%, Can inhibit at least 20% of retinal esterification reactions catalyzed by ^ RAT or ARAT. These effects are not only greater than those of retinol or its esters alone, but also greater than those of combining these two ingredients to produce an additive effect on keratin cells similar to that of retinoid. Examples 3-8 are examples of the compositions of the present invention. These compositions can be prepared according to conventional methods, which are suitable for cosmetic use. In particular, these compositions are suitable for gradation, thick seam, drying, cracking, In the use of aging or damaged skin to improve the appearance and touch of the skin, the composition of the present invention is suitable for -20- the paper rule iUiTssi home standard (CNS) 7 ^ 721GX297 mm) 541182
7 B 五、發明説明(18) 合於使用於健康之皮膚上,以避免或延遲衰老現象。 實例3 此實例係例示併入本發明組合物之高内相油包水乳液。 (請先閱讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印製 此實例係例示併入本發明組合物之水包油面霜。 %w/w 視網醇 0.15 礦物油 4 熊果酸 1 Brij 561 4 Alfol 16RO1 4 三乙醇胺 0.75 -21 - %w/w 視網醇 0.5 全氫化揶子油 3.9 熊果酸 5 Brij 921 5 B entone 3 8 0.5 MgS047H20 0.3 丁基化羥甲酮 0.01 香水 適量 水 至100 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 17 B V. Description of the invention (18) Suitable for use on healthy skin to avoid or delay aging. Example 3 This example illustrates a high internal phase water-in-oil emulsion incorporated into the composition of the present invention. (Please read the notes on the back before filling this page) Printed by the Consumer Cooperatives of the Central Bureau of Standards, Ministry of Economic Affairs This example is an example of an oil-in-water cream that incorporates the composition of the present invention. % w / w Retinol 0.15 Mineral oil 4 Ursolic acid 1 Brij 561 4 Alfol 16RO1 4 Triethanolamine 0.75 -21-% w / w Retinol 0.5 Fully hydrogenated gardenia oil 3.9 Ursolic acid 5 Brij 921 5 B entone 3 8 0.5 MgS047H20 0.3 Butylated hydroxymethyl ketone 0.01 Perfume amount of water to 100 This paper size applies Chinese National Standard (CNS) A4 specification (210X 297 mm) 1
Brij 92係聚環氧乙烯⑵油醯醚。 實例4 541182Brij 92 series poly (ethylene oxide) olein. Example 4 541182
A B 五、發明説明(19) 1,3-丁二醇 3 黃原膠 0.3 香水 適量 丁基化羥甲酮 0.01 水 至100 *Brij 56係十六醇POE (10)。 Alfol 16RO係十六醇。 宥例5 此實例係例示本發明之含醇乳液。 %w/w 棕櫚酸視網酯 0.15 熊果酸 0.1 乙醇 40 香水 適量 丁基化羥甲酮 0.01 水 至100 實例6 (請先閱讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印製 此實例係例示包含本發明組合物之另一種含醇乳液。 %w/w 視網醇 0.15 熊果酸 0.1 乙醇 40 抗氧化劑 0.1 -22- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 541182A B V. Description of the invention (19) 1,3-butanediol 3 Xanthan gum 0.3 Perfume Amount Butyl hydroxymethanone 0.01 Water to 100 * Brij 56 series cetyl alcohol POE (10). Alfol 16RO is cetyl alcohol. Example 5 This example illustrates the alcohol-containing emulsion of the present invention. % w / w Retinyl palmitate 0.15 Ursolic acid 0.1 Ethanol 40 Percent of butylated hydroxymethyl ketone 0.01 Water to 100 Example 6 (Please read the precautions on the back before filling this page) Employees of the Central Bureau of Standards, Ministry of Economic Affairs Printed by a cooperative This example illustrates another alcohol-containing emulsion containing a composition of the present invention. % w / w Retinol 0.15 Ursolic acid 0.1 Ethanol 40 Antioxidant 0.1 -22- This paper size applies to China National Standard (CNS) A4 (210X 297 mm) 541182
A B 經濟部中央標準局員工消費合作社印製 五、發明説明(20) 此實例係例示併入本發明組合物之防曬霜。 %w/w 棕櫊酸視網酯 0.01 熊果酸 0.1 石夕酉同油2 0 0 c t s 7.5 甘油單硬脂酸酯 3 十六烷基硬脂酸醇 1.6 聚環氧乙烯-(20)-十六烷醇 1.4 黃原膠 0.5 Parsol 1789 1.5 戊基甲氧基琥珀酸酯(Parsol MCX) 7 香水 適量 色素 適量 水 至100 實例8 此實例係例示併入本發明組合物之非水性皮膚調理組合 物。 %w/w 視網酸 0.15 齊墩果酸 1 -23- (請先閱讀背面之注意事項再填寫本頁) 香水 適量 水 至100 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐) 541182A B Printed by the Consumers' Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs 5. Description of the Invention (20) This example illustrates the sunscreen incorporated in the composition of the present invention. % w / w Retinyl palmitate 0.01 Ursolic acid 0.1 Shixiong with oil 2 0 0 cts 7.5 Glyceryl monostearate 3 Cetyl stearate 1.6 Poly (ethylene oxide)-(20)- Cetyl Alcohol 1.4 Xanthan Gum 0.5 Parsol 1789 1.5 Amyl Methoxy Succinate (Parsol MCX) 7 Perfume Moderate Pigment Moderate Water to 100 Example 8 This example illustrates a non-aqueous skin conditioning combination incorporated into the composition of the present invention Thing. % w / w retinoic acid 0.15 oleanolic acid 1 -23- (Please read the precautions on the back before filling in this page) Perfume amount of water to 100 This paper size applies Chinese National Standard (CNS) A4 specification (210X 297) %) 541182
A B 五、發明説明(21 ) 矽酮膠SE-301 10 矽酮流體3452 20 矽酮流體3443 55.79 角鯊晞 10 羊毛脂 0.01 膽固醇 0.03 2-羥基-n-辛酮酸 0.7 維他命Ε羊毛醯脂 0.5 草油 0.5 乙醇 2 二甲矽酮聚合物,其具有至少50,000之分子量,及於 25°C下至少10,000分托之黏度,購自GEC公司。 二甲石夕酮環狀五聚物,購自Dow Corning公司。 二甲石夕酉同環狀四聚物,購自D 〇 w C 〇 r n i n g公司。 ------------^---:.11------0 (請先閲讀背面之注意事項再填寫本頁) 經濟部中央標準局員工消費合作社印製 -24- 本紙張尺度適用中國國家標準(CNS ) A4規格(210X 297公釐)AB 5. Description of the invention (21) Silicone glue SE-301 10 Silicone fluid 3452 20 Silicone fluid 3443 55.79 Squalin 10 Lanolin 0.01 Cholesterol 0.03 2-Hydroxy-n-octanoic acid 0.7 Vitamin E Lanolin 0.5 Grass oil 0.5 ethanol 2 dimethyl silicone polymer, which has a molecular weight of at least 50,000 and a viscosity of at least 10,000 d Torr at 25 ° C, was purchased from GEC. Dimethyxone cyclic pentamer was purchased from Dow Corning. Dimethyxene is a cyclic tetramer and was purchased from Dow C O r n i n g. ------------ ^ --- :. 11 ------ 0 (Please read the notes on the back before filling out this page) Printed by the Staff Consumer Cooperative of the Central Standards Bureau of the Ministry of Economic Affairs- 24- This paper size applies to China National Standard (CNS) A4 (210X 297mm)
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JPS5857307A (en) * | 1981-09-30 | 1983-04-05 | Pola Chem Ind Inc | Cosmetic |
US5166176A (en) * | 1986-12-29 | 1992-11-24 | Obagi Zein E | Composition for healing damaged skin |
CA2044162A1 (en) * | 1989-10-13 | 1991-04-14 | Jacques Borg | Long-chained fatty alcohol derivatives, their applications, specifically as cytotrphic and cytoprotecting molecules, and pharmaceutical compounds containing same |
JP3144155B2 (en) * | 1993-05-20 | 2001-03-12 | キヤノン株式会社 | Focus detection device |
FI102247B (en) * | 1993-09-01 | 1998-11-13 | Univ Helsinki Licensing | A process for preparing a stable composition containing wheatgrass juice |
WO1996007396A2 (en) * | 1994-09-07 | 1996-03-14 | Johnson & Johnson Consumer Products, Inc. | Retinoid compositions |
US5529769A (en) * | 1994-12-20 | 1996-06-25 | Chesebrough-Pond's Usa Co., Division Of Conopco, Inc. | Cosmetic compositions containing betulinic acid |
US5560917A (en) * | 1995-02-01 | 1996-10-01 | Maybelline Intermediate Company | Cosmetic makeup composition |
US5523090A (en) * | 1995-02-24 | 1996-06-04 | Chesebrough-Pond's Usa Co., Division Of Conopco, Inc. | Skin treatment composition |
US5536740A (en) * | 1995-06-01 | 1996-07-16 | Elizabeth Arden Company, Division Of Conopco, Inc. | Skin care compositions containing dimethyl imidazolidinone and retinol or retinyl ester |
-
1996
- 1996-09-27 US US08/721,878 patent/US5723139A/en not_active Expired - Fee Related
-
1997
- 1997-09-18 CZ CZ19991088A patent/CZ289876B6/en not_active IP Right Cessation
- 1997-09-18 ID IDW990125A patent/ID21761A/en unknown
- 1997-09-18 JP JP10515236A patent/JP2000503030A/en not_active Ceased
- 1997-09-18 EP EP97910309A patent/EP0975319B1/en not_active Expired - Lifetime
- 1997-09-18 KR KR1019997002653A patent/KR100320138B1/en not_active IP Right Cessation
- 1997-09-18 BR BR9712135-5A patent/BR9712135A/en not_active IP Right Cessation
- 1997-09-18 AU AU47755/97A patent/AU714984B2/en not_active Ceased
- 1997-09-18 RU RU99108678/14A patent/RU2175546C2/en not_active IP Right Cessation
- 1997-09-18 WO PCT/EP1997/005139 patent/WO1998013019A1/en active IP Right Grant
- 1997-09-18 PL PL97332547A patent/PL332547A1/en unknown
- 1997-09-18 CN CN97199920A patent/CN1237897A/en active Pending
- 1997-09-18 DE DE69720539T patent/DE69720539T2/en not_active Expired - Fee Related
- 1997-09-18 CA CA002266615A patent/CA2266615A1/en not_active Abandoned
- 1997-09-24 IN IN550BO1997 patent/IN189578B/en unknown
- 1997-09-26 ZA ZA978658A patent/ZA978658B/en unknown
- 1997-09-29 AR ARP970104471A patent/AR009098A1/en unknown
- 1997-12-16 TW TW086118988A patent/TW541182B/en active
Also Published As
Publication number | Publication date |
---|---|
KR100320138B1 (en) | 2002-01-12 |
CZ289876B6 (en) | 2002-04-17 |
EP0975319B1 (en) | 2003-04-02 |
AU714984B2 (en) | 2000-01-13 |
CN1237897A (en) | 1999-12-08 |
CZ108899A3 (en) | 1999-08-11 |
BR9712135A (en) | 1999-08-31 |
KR20000048698A (en) | 2000-07-25 |
PL332547A1 (en) | 1999-09-13 |
AU4775597A (en) | 1998-04-17 |
ID21761A (en) | 1999-07-22 |
CA2266615A1 (en) | 1998-04-02 |
RU2175546C2 (en) | 2001-11-10 |
EP0975319A1 (en) | 2000-02-02 |
ZA978658B (en) | 1999-03-26 |
DE69720539T2 (en) | 2004-04-29 |
US5723139A (en) | 1998-03-03 |
IN189578B (en) | 2003-03-29 |
DE69720539D1 (en) | 2003-05-08 |
WO1998013019A1 (en) | 1998-04-02 |
AR009098A1 (en) | 2000-03-08 |
JP2000503030A (en) | 2000-03-14 |
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